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66

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2320	Indacaterol	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Indacaterol 是一种超长效β-肾上腺素受体激动剂。
T15108	DG-041	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	DG-041 是高亲和力，选择性的，有效的 EP3受体拮抗剂，在结合和 FLIPR 试验中，IC50分别为 4.6 nM 和 8.1 nM。DG-041通过抑制 PGE2促进血小板聚集。DG-041具有血脑屏障渗透性。
T4330	CaCCinh-A01	Chloride channel	Membrane transporter/Ion channel
	CaCCinh-A01 是钙激活氯离子通道和TMEM16A 抑制剂，IC50值分别为 10 和 2.1 μM。
T15418	GS-6201 CVT-6883	Adenosine Receptor	GPCR/G Protein; Neuroscience
	GS-6201 (CVT-6883) 是选择性腺苷 A2B 受体拮抗剂。它对人腺苷 A2B 受体具有高亲和力和选择性 (Ki=22 nM)。它降低了小鼠急性心肌梗死后心脏中 caspase-1 的活性，并减弱了心脏重塑。它减弱了致敏小鼠 NECA，AMP 或变应原诱导的气道反应性。
T5329	Trandolapril	Angiotensin-converting Enzyme (ACE)	Metabolism
	Trandolapril 是 Trandolaprilat 的前体药物。Trandolapril 是一种口服血管紧张素转换酶抑制剂，在高血压和充血性心力衰竭及心肌梗死领域有研究价值。
T1239	Indacaterol maleate 马来酸茚达特罗,QAB149	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Indacaterol maleate (QAB149) 是一种超长效的 β-肾上腺素受体激动剂。
T1479	Isosorbide dinitrate 硝酸异山梨酯,Isordil,Nitrosorbide,Sorbide nitrate,Sorbidnitrate	Others; NO Synthase	Immunology/Inflammation; Others
	Isosorbide dinitrate (Isordil) 是 NO 供体，可预防心肌梗死 (MI) 引起的左室重构及心功能退化。
T7714	Temocapil	Tyrosinase	Proteases/Proteasome
	Temocapil 是一种酪氨酸激酶抑制剂。
T3461	Losartan Carboxylic Acid EXP-3174,E-3174	RAAS	Endocrinology/Hormones
	Losartan Carboxylic Acid (E-3174) 是 Losartan 的活性羧酸代谢产物，是血管紧张素Ⅱ受体 1 型(AT1)拮抗剂。它能够阻断血管紧张素 II 诱导的血管平滑肌细胞反应，可以提高血浆肾素活性，降低平均动脉压。
T3230	NLRP3-IN-2 5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide,4-[2-(5-氯-2-甲氧基苯甲酰氨基)乙基]苯磺酰胺,NLRP3 Inflammasome Inhibitor I	NOD-like Receptor (NLR); NOD	Immunology/Inflammation; NF-κB
	NLRP3-IN-2 (5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide) 是一种能够合成格列本脲的中间物，对心肌细胞中NLRP3炎症小体的形成具有抑制作用，在小鼠心肌缺血/再灌注后限制梗死面积，且对代谢无影响。
T6698	Temocapril hydrochloride CS-622 HCl,Acecol,Temocapril HCl,CS-622,盐酸替莫普利	RAAS	Endocrinology/Hormones
	Temocapril hydrochloride (CS-622 HCl) 是血管紧张素转化酶 (ACE) 抑制剂。Temocapril HCl 能够用于充血性心力衰竭、急性心肌梗死、高血压、胰岛素抵抗和肾脏疾病的研究。
T11239	Ethacizine hydrochloride NIK-244,Ethacizin,NIK-244 hydrochloride	Sodium Channel	Membrane transporter/Ion channel
	Ethacizine hydrochloride (NIK-244) 具有抗心律失常活性，其作用于心脏活动有关，可用于研究心律失常和心肌梗死。
T67941	PDE5-IN-9
	PDE5-IN-9对Phosphodiesterase PDE1c 具有抑制作用，可用来治疗高血压、心力衰竭、心肌梗塞、肾衰竭、哮喘、支气管炎和痴呆。
T24115	GSK854 GSK-854,GSK 854	Apoptosis	Apoptosis
	GSK854 是一种具有高选择性和有效性的肌钙蛋白 I 相互作用激酶 (TNNI3K) 抑制剂，抑制小鼠心肌梗死损伤细胞焦亡和细胞凋亡，可限制缺血性心脏的氧化应激、损伤和不良重塑。
T68022L	Sulotroban potassium BM 13177 potassium,Sulotroban potassium(72131-33-0 Free base)	PPAR	DNA Damage/DNA Repair; Metabolism
	Sulotroban potassium 是一种小分子血栓素A2受体（TXA2R）拮抗剂，可用于研究心肌梗塞和血栓形成。
T0407	Edaravone 依达拉奉右莰醇,依达拉奉,MCI-186	Apoptosis; MMP; Free radical scavengers	Apoptosis; oxidation-reduction; Proteases/Proteasome
	Edaravone (MCI-186) 是一种新型自由基清除剂，能够抑制大鼠与 MMP-9有关的脑出血。
T12078	ML334 LH601A	Nrf2	Immunology/Inflammation
	ML334 (LH601A) 是一种可穿过细胞膜且具有有效性的 NRF2 激活剂，抑制 Keap1-NRF2 蛋白质相互作用，抑制心脏成纤维细胞活化和增殖来改善心肌梗死诱导的心脏纤维化。
T77611	DAPK-IN-2 WAY-380496	DAPK	Apoptosis
	DAPK-IN-2 (WAY-380496) 是一种 DAPK 抑制剂。 DAPK-IN-2 具有潜在的抗癌活性，可调节细胞发生自噬反应，可用于研究脑梗死和缺血性疾病。
TP2279L	Obestatin (rat) acetate	GHSR	GPCR/G Protein
	Obestatin (rat) acetate 是 G 蛋白偶联受体 39 (GPR39) 的内源性配体。它具有抗炎、抗心肌梗塞和抗氧化特性。它抑制食物摄入，抑制空肠收缩，并减少体重增加。
T0230	Prasugrel LY640315,CS-747,普拉格雷,PCR 4099	P2Y Receptor	GPCR/G Protein; Neuroscience
	Prasugrel (CS-747) 是一种噻吩吡啶和前药，是一种可口服的 P2Y12受体拮抗剂，抑制 ADP 诱导的血小板聚集，用于预防急性冠状动脉综合征患者的血栓形成、不稳定型心绞痛和心肌梗塞，以及接受经皮冠状动脉介入治疗的患者。
T39115	ABR-238901	TLR	Immunology/Inflammation
	ABR-238901是一种可口服的、有作用的 S100A8/A9阻滞剂，对 S100A8/A9与其受体 RAGE(晚期糖基化终产物受体)和TLR4 (toll 样受体4)的相互作用具有抑制作用。ABR-238901具有作为治疗心肌梗死(MI)化合物的潜力。
T31206	Darexaban YM 150,Darexaban, Tanexaban,YM150	Factor Xa	Metabolism
	Darexaban (Tanexaban, YM-150) 是选择性的、口服具有活力的 Xa 因子 (FXa) 抑制剂，IC50=54.6 nM。它对其他相关丝氨酸蛋白酶(如胰蛋白酶、凝血酶和激肽释放酶)具有高选择性。它具有抗凝和抗血栓形成作用。
T36008	Nebentan potassium
	Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan potassium inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan potassium inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB re...
T22323	Enoxaparin sodium	Thrombin	Proteases/Proteasome
	Enoxaparin sodium 是一种低分子量肝素 (LMWH)，已获得美国 FDA 批准，可用于医疗管理的 ST 段心肌梗死 (STEMI) 或 STEMI 及随后的经皮冠状动脉介入治疗 (PCI) 患者。它与抗凝血酶结合并增强其作用，并抑制凝血因子 XIa、IXa、Xa 和 IIa（凝血酶），从而防止血栓形成。
T36569	KR-32568	Sodium Channel	Membrane transporter/Ion channel
	KR-32568是一种钠/氢交换器1（NHE-1）抑制剂（IC50：230 nM）。KR-32568具有强大的心脏保护作用。当使用浓度为10μM 时，它能在离体的缺血大鼠心脏模型中恢复心脏收缩功能。KR-32568（0.3mg/kg）在缺血和再灌注损伤的大鼠模型中减少了心肌梗死的大小。
T24873	TGX-115 TGX 115	PI3K	PI3K/Akt/mTOR signaling
	TGX-115是一种细胞渗透性和有效的PI 3-K 异构体p110β/p110δ抑制剂(对p110β IC50值为 0.13 μM, 对p110δ值为0.63 μM），是一种调节血小板粘附过程的酶，可抑制磷酸肌苷（PI）3-激酶，可用来治疗冠状动脉闭塞、中风、急性冠状动脉综合征、急性心肌梗塞、血管再狭窄、动脉硬化和不稳定心绞痛等心血管疾病。
T14390L	(2R,3S)-Azelaprag	Apelin receptor	GPCR/G Protein
	(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide 是一种Apelin 受体激动剂，对Apelin 受体的EC50为0.012 µM。(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide 可用于治疗心力衰竭、动脉粥样硬化、肥胖、糖尿病、肌萎缩侧索硬化、冠心病、高血压、中风和心肌梗塞等疾病。
T34327	Ridogrel R-70416,R 68070,R-68070,R70416,R 70416,R68070
	Lidogrell is a dual-acting agent that can be used to prevent systemic thromboembolism and as an adjunct to thrombolytic therapy in acute myocardial infarction.
T21206	Triphenyltetrazolium bromide AI3-62388
	Triphenyltetrazolium bromide may be used to detect experimental cerebral infarction and biochemical analysis.
T28130	Naltiazem RO 236152,RO-236152,RO236152
	Naltiazem, a calcium channel antagonist, is used potentially for the treatment of arrhythmias, hypertension and myocardial infarction.
T27581	Icrocaptide ITF 1697,ITF-1697,ITF1697
	Icrocaptide is used potentially for the treatment of acute myocardial infarction.
T24746	Zalunfiban RUC4,RUC 4,RUC-4
	RUC-4 is an aIIb 3 antagonist. It is also used for prehospital therapy of myocardial infarction.
T69078	Tiapamil Free Base
	Tiapamil Free Base is a phenylethylamine derivative that acts as a calcium antagonist showing hemodynamic effects in patients with acute myocardial infarction.
T37697	D-GsMTx4 D-GsMTx4
	TRPC1/6 and Piezo2 inhibitor. Exhibits same effect as L-enantiomer, GsMTx4 (Cat. No. 4912) on TRPC channels. Inhibits mechanosensitive currents by ~70%. Protects against myocardial infarction in mouse ischemia/reperfusion model. Resistant to proteolytic digestion.
T22685	CP-471474 CP 471474	Others	Others
	Broad spectrum MMP inhibitor (IC<sub>50</sub> values are 0.7, 0.9, 13, 16 and 1170 nM for MMP-2, MMP-13, MMP-9, MMP-3 and MMP-1 respectively). Attenuates early left ventricular dilation after experimental myocardial infarction in mice.
T62878	Zalunfiban dihydrochloride
	Zalunfiban (RUC-4) dihydrochloride 是一种选择性的、有效的血小板αIIbβ3拮抗剂，其 IC50 值为 45 nM。Zalunfiban dihydrochloride 能够用于研究心肌梗死。
T73240	PDE5-IN-4
	PDE5-IN-4为磷酸二酯酶5（PDE5）抑制剂，应用于急性心肌梗死及再灌注损伤、消化系统疾病、糖尿病相关损害及肝功能衰竭的研究。
T73661	Delcasertib hydrochloride
	Delcasertib (KAI-9803) hydrochloride 是有效，选择性的 δ 蛋白激酶 C (δPKC) 抑制剂。Delcasertib (KAI-9803) hydrochloride 可改善急性心肌梗死动物模型的缺血再灌注损伤。
T69000	Prenalterol hydrochloride
	Prenalterol hydrochloride is a partial adrenergic agonist with functional beta 1-receptor specificity and inotropic effect. It is effective in the treatment of acute cardiac failure, postmyocardial infarction low-output syndrome, shock, and reducing orthostatic hypotension in the Shy-Drager syndrome.
T71800	Metoprolol HCl
	Metoprolol is a selective β1 receptor blocker medication. It is used to treat high blood pressure, chest pain due to poor blood flow to the heart, and a number of conditions involving an abnormally fast heart rate. It is also used to prevent further heart problems after myocardial infarction and to prevent headaches in those with migraines.
T78026	LQVTDSGLYRCVIYHPP TFA
	LQVTDSGLYRCVIYHPP (LP17) TFA 是一种针对髓系细胞表面的触发受体1 (TREM-1) 的抑制肽。该化合物能有效减缓缺血导致的梗塞及神经元损害，并可穿透血脑屏障，阻断 TREM-1的活性。
T61540	F15845
	F 15845 is a potent and persistent blocker of the sodium current. It possesses cardioprotective properties and exhibits both anti-ischemic activity and short- and long-term cardioprotection following myocardial infarction. Furthermore, F 15845 finds utility in the investigation of myocardial functional impairment [1].
T11448	GOAT-IN-1	Others	Others
	GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of diabetes, hyperlipidemia, non-alcoholic fatty liver, Alzheimer’s disease, Parkinson’s disease, cerebrovascular dementia, cerebral infa
T62507	Protease-Activated Receptor-1 antagonist 1
	Protease-Activated Receptor-1 antagonist 1 (Compound 13) 是一种蛋白酶激活受体 1 (PAR-1) 拮抗剂，通过 FLIPR 技术得到的 IC50 为 3 nM。Protease-Activated Receptor-1 antagonist 1 能够用于研究血栓性心血管、心肌梗塞和外周动脉疾病。
T77026	Goflikicept
	Goflikicept (RPH 104) 是一种可选择性结合并灭活循环中的 IL-1ß 和 IL-1α 的杂合蛋白。此化合物在研究ST段抬高型心肌梗死（STEMI）方面具有潜力。
T78025	LQVTDSGLYRCVIYHPP
	LQVTDSGLYRCVIYHPP (LP17) 为髓系细胞表达之触发受体 1 (TREM-1) 抑制性肽类化合物，能有效减轻缺血引发的梗塞及神经元损害，并可渗透大脑，阻断TREM-1。
T64084	Clazosentan
	Clazosentan (Ro 61-1790) 是内皮素 A 受体 (ETAreceptor) 的选择性拮抗剂，对 ET-1 介导的血管收缩表现出抑制作用。Clazosentan 能够预防脑血管痉挛、血管痉挛相关性脑梗死。
T77166	Rovelizumab
	Rovelizumab是一种针对CD11/CD18细胞粘附蛋白的人源化单克隆抗白细胞整合素抗体，主要用于多发性硬化症(MS)、失血性休克、心肌梗死(MI)和中风研究。
T77163	Pexelizumab
	Pexelizumab (h5G1.1-SC)为一种针对C5补体成分的人源化单克隆抗体。该化合物可抑制凋亡(apoptosis)和白细胞浸润，常用于研究脑缺血再灌注损伤和心肌梗死。
T38800	MMPI-1154
	MMPI-1154 is a highly promising imidazole-carboxylic acid (ICA) MMP-2 inhibitor (IC 50 = 6.6 μM) with excellent cardio-cytoprotective properties. It is specifically designed for the study of acute myocardial infarction. Additionally, MMPI-1154 exhibits significant inhibitory effects on MMP-13, MMP-1, and MMP-9 activities with IC 50 values of 1.8 μM, 10 μM, and 13 μM, respectively.

化合物

Cat.No: T2320

Target: Adrenergic Receptor

Cat.No: T15108

Target: Prostaglandin Receptor

Cat.No: T4330

Target: Chloride channel

Cat.No: T15418

Synonym: CVT-6883

Target: Adenosine Receptor

Cat.No: T5329

Target: Angiotensin-converting Enzyme (ACE)

Indacaterol maleate

Cat.No: T1239

Synonym: 马来酸茚达特罗,QAB149

Target: Adrenergic Receptor

Isosorbide dinitrate

Cat.No: T1479

Synonym: 硝酸异山梨酯,Isordil,Nitrosorbide,Sorbide nitrate,Sorbidnitrate

Target: Others, NO Synthase

Cat.No: T7714

Target: Tyrosinase

Losartan Carboxylic Acid

Cat.No: T3461

Synonym: EXP-3174,E-3174

Target: RAAS

Cat.No: T3230

Synonym: 5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide,4-[2-(5-氯-2-甲氧基苯甲酰氨基)乙基]苯磺酰胺,NLRP3 Inflammasome Inhibitor I

Target: NOD-like Receptor (NLR), NOD

Temocapril hydrochloride

Cat.No: T6698

Synonym: CS-622 HCl,Acecol,Temocapril HCl,CS-622,盐酸替莫普利

Target: RAAS

Ethacizine hydrochloride

Cat.No: T11239

Synonym: NIK-244,Ethacizin,NIK-244 hydrochloride

Target: Sodium Channel

Cat.No: T67941

Cat.No: T24115

Synonym: GSK-854,GSK 854

Target: Apoptosis

Sulotroban potassium

Cat.No: T68022L

Synonym: BM 13177 potassium,Sulotroban potassium(72131-33-0 Free base)

Target: PPAR

Cat.No: T0407

Synonym: 依达拉奉右莰醇,依达拉奉,MCI-186

Target: Apoptosis, MMP, Free radical scavengers

Cat.No: T12078

Synonym: LH601A

Target: Nrf2

Cat.No: T77611

Synonym: WAY-380496

Target: DAPK

Obestatin (rat) acetate

Cat.No: TP2279L

Target: GHSR

Cat.No: T0230

Synonym: LY640315,CS-747,普拉格雷,PCR 4099

Target: P2Y Receptor

Cat.No: T39115

Target: TLR

Cat.No: T31206

Synonym: YM 150,Darexaban, Tanexaban,YM150

Target: Factor Xa

Nebentan potassium

Cat.No: T36008

Enoxaparin sodium

Cat.No: T22323

Target: Thrombin

Cat.No: T36569

Target: Sodium Channel

Cat.No: T24873

Synonym: TGX 115

Target: PI3K

(2R,3S)-Azelaprag

Cat.No: T14390L

Target: Apelin receptor

Cat.No: T34327

Synonym: R-70416,R 68070,R-68070,R70416,R 70416,R68070

Triphenyltetrazolium bromide

Cat.No: T21206

Synonym: AI3-62388

Cat.No: T28130

Synonym: RO 236152,RO-236152,RO236152

Cat.No: T27581

Synonym: ITF 1697,ITF-1697,ITF1697

Cat.No: T24746

Synonym: RUC4,RUC 4,RUC-4

Tiapamil Free Base

Cat.No: T69078

Cat.No: T37697

Synonym: D-GsMTx4

Cat.No: T22685

Synonym: CP 471474

Target: Others

Zalunfiban dihydrochloride

Cat.No: T62878

Cat.No: T73240

Delcasertib hydrochloride

Cat.No: T73661

Prenalterol hydrochloride

Cat.No: T69000

Cat.No: T71800

LQVTDSGLYRCVIYHPP TFA

Cat.No: T78026

Cat.No: T61540

Cat.No: T11448

Target: Others

Protease-Activated Receptor-1 antagonist 1

Cat.No: T62507

Cat.No: T77026

LQVTDSGLYRCVIYHPP

Cat.No: T78025

Cat.No: T64084

Cat.No: T77166

Cat.No: T77163

Cat.No: T38800

Cat. No.	Product Name	Target	Signaling Pathways
T2893	Muscone 3-Methylcyclopentadecanone,Methylexaltone,麝香酮	MMP; TNF; NF-κB; NOD-like Receptor (NLR); P-gp; Interleukin	Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; NF-κB; Proteases/Proteasome
	Muscone (3-Methylcyclopentadecanone) 是中药麝香的一种主要活性单体。它抑制NF-κB 和NLRP3炎性小体的活化，显著降低炎性细胞因子水平，并最终改善心脏功能和存活率。
T3S0289	Araloside X	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Aralosides possess protective effect against experimental myocardial ischemia and infarction, the mechanism of myocardial protection may be attributed to the amelioration of FFA metabolic deterioration and membrane peroxidation induced by oxygen free radi

天然产物

Cat.No: T2893

Synonym: 3-Methylcyclopentadecanone,Methylexaltone,麝香酮

Target: MMP, TNF, NF-κB, NOD-like Receptor (NLR), P-gp, Interleukin

Cat.No: T3S0289

Target: Calcium Channel

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